FSL0499
- Structure
- InChI=1S/C15H23NO4/c1-8-3-9(2)15(20)11(4-8)12(17)5-10-6-13(18)16-14(19)7-10/h8-12,17H,3-7H2,1-2H3,(H,16,18,19)/t8-,9-,11-,12+/m0/s1
- InChIKey=YPHMISFOHDHNIV-FSZOTQKASA-N
- Synonyms
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- 66-81-9
- A-67
- Acti-Aid
- Actidione
- Cycloheximide
- Cycloheximide
- D-73-2
- GS-700-II
- Naramycin
- Naramycin-A
- NSC-185
- P-42-A
- Zygomycin-D
- Origin
- Streptomyces griseus
- Biological activities
- Inhibition of eukariotic protein synthesis
- Therapeutic
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Anticancer
Antifungal
- Target
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60S ribosomes
- Assay information
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Inhibitor of protein synthesis in eukaryotes, and works as an antifungal antibiotics
Reduction of the context of total nuclear ribonucleoprotein complexes at non-lethal dose of rat liver (2 mg/kg body weight)
Inhibitor of protein synthesis in rat liver (2-5 mg/kg body weight)
Inducer of apotosis in HL-60 cells, T cell hybridomas, Burkitt’s lymphoma cells, and other cell types
Inhibitor of hFKBP12, peptidyl-prolyl isomerase (PPIase) (Ki = 3.4 μM)
Binding to the tRNA E-site of the 60S subunit
- References
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Klinge S, Voigts-Hoffmann F, Leibundgut M, Arpagaus S, Ban N
Crystal structure of the eukaryotic 60S ribosomal subunit in complex with initiation factor 6.
Science, 334(6058): 941-948 (2011) 22052974 doi: 10.1126/science.1211204
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Schneider-Poetsch T, Ju J, Eyler DE, Dang Y, Bhat S, Merrick WC, Green R, Shen B, Liu JO
Inhibition of eukaryotic translation elongation by cycloheximide and lactimidomycin.
Nat Chem Biol, 6(3): 209-217 (2010) 20118940 doi: 10.1038/nchembio.304
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Christner C, Wyrwa R, Marsch S, Küllertz G, Thiericke R, Grabley S, Schumann D, Fischer G
Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
J Med Chem, 42(18): 3615-3622 (1999) 10479292 doi: 10.1021/jm991038t
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Lotem J, Sachs L
Regulation of bcl-2, bcl-XL and bax in the control of apoptosis by hematopoietic cytokines and dexamethasone.
Cell Growth Differ, 6(6): 647-653 (1995) 7669718
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Grand RJ, Milner AE, Mustoe T, Johnson GD, Owen D, Grant ML, Gregory CD
A novel protein expressed in mammalian cells undergoing apoptosis.
Exp Cell Res, 218(2): 439-451 (1995) 7796880 doi: 10.1006/excr.1995.1177
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Chow SC, Peters I, Orrenius S
Reevaluation of the role of de novo protein synthesis in rat thymocyte apoptosis.
Exp Cell Res, 216(1): 149-159 (1995) 7813615 doi: 10.1006/excr.1995.1019
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Stoyanova BB, Hadjiolov AA
Alterations in the processing of rat-liver ribosomal RNA caused by cycloheximide inhibition of protein synthesis.
Eur J Biochem, 96(2): 349-356 (1979) 456380
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Ch'ih JJ, Duhl DM, Faulkner LS, Devlin TM
Regulation of mammalian protein synthesis in vivo. Simulated transport of nuclear ribonucleoprotein complexes to the cytoplasm after cycloheximide treatment.
Biochem J, 178(3): 643-649 (1979) 454372
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J. Bacteriol., 56: 283 (1948)
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J. Bacteriol., 56: 283 (1948)
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J. Am. Chem. Soc., 69: 474 (1947)